24730-88-9Relevant academic research and scientific papers
Divergent Total Syntheses of Yaequinolone-Related Natural Products by Late-Stage C-H Olefination
Ces, Sabela Vega,Fernández-Ibá?ez, M. ángeles,Jia, Wen-Liang
supporting information, p. 6259 - 6277 (2021/05/29)
Divergent total syntheses of 10 yaequinolone-related natural products have been achieved for the first time by late-stage C-H olefination of 3,4-dioxygenated 4-aryl-5-hydroxyquinolin-2(1H)-ones, core structures of this family of natural products. A robust synthetic methodology to construct the core structures has been established, and the C-H olefination reaction has been carried out with synthetically useful yields and high levels of site-selectivity under mild reaction conditions in the presence of a Pd/S,O-ligand catalyst.
ONO-8430506: A Novel Autotaxin Inhibitor That Enhances the Antitumor Effect of Paclitaxel in a Breast Cancer Model
Hiramatsu, Atsushi,Hirooka, Yasuo,Hisaichi, Katsuya,Imagawa, Akira,Iwaki, Yuzo,Katoh, Makoto,Kobayashi, Juta,Komichi, Yuka,Maeda, Tatsuo,Matsumura, Naoya,Moriguchi, Hideki,Nakatani, Shingo,Nishiyama, Taihei,Ohhata, Akira,Okabe, Yasuyuki,Okada, Masahiro,Ota, Hiroto,Saga, Hiroshi,Sugiyama, Tetsuya,Watanabe, Toshihide,Yamamoto, Shingo
supporting information, p. 1335 - 1341 (2020/07/06)
Lysophosphatidic acid (LPA) is a bioactive lipid mediator that elicits a number of biological functions, including smooth muscle contraction, cell motility, proliferation, and morphological change. LPA is endogenously produced by autotaxin (ATX) from extracellular lysophosphatidylcholine (LPC) in plasma. Herein, we report our medicinal chemistry effort to identify a novel and highly potent ATX inhibitor, ONO-8430506 (20), with good oral availability. To enhance the enzymatic ATX inhibitory activity, we designed several compounds by structurally comparing our hit compound with the endogenous ligand LPC. Further optimization to improve the pharmacokinetic profile and enhance the ATX inhibitory activity in human plasma resulted in the identification of ONO-8430506 (20), which enhanced the antitumor effect of paclitaxel in a breast cancer model.
ETHANEDIAMINE-HETEROCYCLE DERIVATIVES AS INHIBITORS OF PROTEIN ARGININE METHYLTRANSFERASES
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Paragraph 0776, (2019/09/15)
The present invention relates to ethanediamine-heterocycle compounds that are able to act as inhibitors of PRMTs (protein arginine methyltransferases) for treating cancer and other diseases mediated by PRMTs.
4,5,6-TRI-SUBSTITUTED INDAZOLES DERIVATIVES, PREPARATION THEREOF, AND USE THEREOF IN MEDICINES
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Paragraph 0161; 0163, (2019/02/19)
Provided are 4,5,6-tri-substituted indazoles derivatives, a preparation method therefor, and a use thereof in medicines. Specifically, provided are compounds of formula (I) or pharmaceutically acceptable salts, stereoisomers, solvates, or prodrugs thereof
TETRAHYDRO-IMIDAZO QUINOLINE COMPOSITIONS AS CBP/P300 INHIBITORS
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Paragraph 0086, (2019/04/11)
The present disclosure is directed to inhibitors of the CBP/p300 family of bromodomains. The compounds can be useful in the treatment of disease or disorders associated with the inhibition of the CBP/p300 family of bromodomains. For instance, the disclosure is concerned with compounds and compositions for inhibition of the CBP/p300 family of bromodomains, methods of treating, preventing, or ameliorating diseases or disorders associated with the inhibition of CBP/p300 family of bromodomains, and methods of synthesis of these compounds.
HETEROARYLDIHYDROPYRIMIDINE DERIVATIVES AND METHODS OF TREATING HEPATITIS B INFECTIONS
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Page/Page column 110; 111, (2019/01/17)
Provided herein are compounds useful for the treatment of HBV infection in a subject in need thereof, pharmaceutical compositions thereof, and methods of inhibiting, suppressing, or preventing HBV infection in the subject.
Solid dispersions containing an apoptosis-inducing agent
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Page/Page column 274, (2019/03/15)
A pro-apoptotic solid dispersion comprises, in essentially non-crystalline form, a Bcl-2 family protein inhibitory compound of Formula I as defined herein, dispersed in a solid matrix that comprises (a) a pharmaceutically acceptable water-soluble polymeric carrier and (b) a pharmaceutically acceptable surfactant. A process for preparing such a solid dispersion comprises dissolving the compound, the polymeric carrier and the surfactant in a suitable solvent, and removing the solvent to provide a solid matrix comprising the polymeric carrier and the surfactant and having the compound dispersed in essentially non-crystalline form therein. The solid dispersion is suitable for oral administration to a subject in need thereof for treatment of a disease characterized by overexpression of one or more anti-apoptotic Bcl-2 family proteins, for example cancer.
PYRAZOLYLAMINOBENZIMIDAZOLE DERIVATIVES AS JAK INHIBITORS
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Page/Page column 19, (2018/03/26)
The present invention provides compounds of the formula below (I'): where R, and R1-R3 are as described herein, methods of treating patients for certain types of autoimmune diseases and cancer, and processes for preparing the compounds.
SUBSTITUTED BICYCLIC PYRAZOLE COMPOUNDS AS RORgammaT INHIBITORS AND USES THEREOF
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Paragraph 0228; 0230, (2018/11/21)
The present invention relates to compounds according to Formula I: and pharmaceutically acceptable salts thereof. Such compounds can be used in the treatment of RORgammaT-mediated diseases or conditions.
As a substituted bicyclic pyrazole compound and use ROR γ T inhibitor
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Paragraph 0182; 0183, (2019/01/10)
The present invention relates to compounds according to Formula I: and pharmaceutically acceptable salts thereof. Such compounds can be used in the treatment of RORgammaT-mediated diseases or conditions.
